Evidence map›Paper›PMID 20942780›Full record

ReviewCurrent drug metabolism2010

Psychedelic 5-methoxy-N,N-dimethyltryptamine: metabolism, pharmacokinetics, drug interactions, and pharmacological actions.

Hong-Wu Shen, Xi-Ling Jiang, Jerrold C Winter, Ai-Ming Yu

Registry-linked trialOpen access · greenAbstract readReview
In one paragraph

Review in Current drug metabolism, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05698095 (A Phase 1, First-in-human, Double-blind, Placebo-controlled, Randomized, Single- and Multiple-ascending-dose Study to Determine the Safety, Tolerability, and Pharmacokinetics of 5-methoxy-N,N-dimethyltryptamine), which is not on this map. Cited by 85 papers, 2 of them syntheses that pooled it.

0numbers the graph read from it
0cells of the map it votes in
85citing papers in PubMed, 2 pooled it
5.5field-weighted citation impact, top 5% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

NCT05698095 phase1completednot on this mapstarted 2022, after this paper: background citation

A Phase 1, First-in-human, Double-blind, Placebo-controlled, Randomized, Single- and Multiple-ascending-dose Study to Determine the Safety, Tolerability, and Pharmacokinetics of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) Administered by Intramuscular Injection in Healthy Subjects

TypeinterventionalSponsorUsona InstituteRan2022 to 2023Enrolled54ConditionsPharmacokinetics, Safety, TolerabilityArms5-methoxy-N,N-dimethyltryptamine succinate salt, Placebo
3 · Its place in the literature

Who cites it

85 citing papers in PubMed, 2 syntheses or guidelines pooled it, 167 citations in OpenAlex.

  1. Pooled it
  2. The pharmacological interaction of compounds in ayahuasca: a systematic review.Revista brasileira de psiquiatria (Sao Paulo, Brazil : 1999)
    Pooled it
  3. Trial
  4. Trial
  5. Review
  6. Review
  7. Article
  8. Trials, trips, and tribulations: pathways for implementing psychedelic therapy in Ireland.The international journal of neuropsychopharmacology · 2026
    Review
  9. Article
  10. Review
  11. Review
  12. Review
  13. Article
  14. Review
  15. Review
  16. Article
  17. Review
  18. The Invasive Mechanism and Impact ofPlants (Basel, Switzerland) · 2025
    Review
  19. Review
  20. Article

25 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors at 1 institution in 1 country.

Hong-Wu ShenDepartment of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, School of Medicine and Biomedical Sciences, University at Buffalo, The State University of New York, Buffalo, NY 14260-1200, USA.
Xi-Ling Jiang
Jerrold C Winter
Ai-Ming Yu
Buffalo State University · US

Funding

Pharmacogenetics in indolealkylamine metabolism and drug interactionsR01DA021172 · NIDA · STATE UNIVERSITY OF NEW YORK AT BUFFALO · PI YU, AIMING · 2007 to 2011
$1.7M
NIDA NIH HHS R01 DA021172NIDA NIH HHS R01DA021172
6 · The paper itself

Abstract

5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metabolite, bufotenine, while it is mainly inactivated through the deamination pathway mediated by monoamine oxidase A (MAO-A). 5-MeO-DMT is often used with MAO-A inhibitors such as harmaline. Concurrent use of harmaline reduces 5-MeO-DMT deamination metabolism and leads to a prolonged and increased exposure to the parent drug 5-MeO-DMT, as well as the active metabolite bufotenine. Harmaline, 5-MeO-DMT and bufotenine act agonistically on serotonergic systems and may result in hyperserotonergic effects or serotonin toxicity. Interestingly, CYP2D6 also has important contribution to harmaline metabolism, and CYP2D6 genetic polymorphism may cause considerable variability in the metabolism, pharmacokinetics and dynamics of harmaline and its interaction with 5-MeO-DMT. Therefore, this review summarizes recent findings on biotransformation, pharmacokinetics, and pharmacological actions of 5-MeO-DMT. In addition, the pharmacokinetic and pharmacodynamic drug-drug interactions between harmaline and 5-MeO-DMT, potential involvement of CYP2D6 pharmacogenetics, and risks of 5-MeO-DMT intoxication are discussed.

Indexed as

AnimalsBufoteninCytochrome P-450 CYP2D6Drug InteractionsHallucinogensHarmalineHumansMethoxydimethyltryptaminesPharmacogeneticsSerotonin Receptor AgonistsBufoteninCytochrome P-450 CYP2D6HallucinogensHarmalineMethoxydimethyltryptaminesSerotonin Receptor Agonists

Identifiers

PMID20942780
PMCPMC3028383
OpenAlexW2126900649

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.